Biphenyl diester liquid medicinal composition containing fat

A technology of bifendate and liquid medicine, which is applied in the direction of drug combination, oil/fat/wax non-active ingredients, emulsion delivery, etc., and can solve the problems of inability to obtain bioavailability, waste, and high treatment cost

Inactive Publication Date: 2004-03-03
佟丽 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of them can obtain ideal bioavailability. Among them, because bifendate is in a highly dispersed state, the in vitro dissolution is relatively high, and the bioavailability is rela

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment one bifendate emulsion No. 1

[0018] Bifendate 2.0g

[0019] soybean oil 180g

[0020] Soy Lecithin 60g

[0021] Sodium deoxycholate 10g

[0022] Deionized water up to 1000ml

[0023] Preparation process: heat the prescribed amount of bifendate, soybean oil, and soybean lecithin to 80°C, and dissolve sodium deoxycholate in 500ml of deionized water at 80°C, add them together to a tissue masher, and stir at a high speed, 8000 RPM, 3 minutes each time, repeated 3 times to obtain a white emulsion. After the emulsion is cooled, add deionized water to 1000ml, and circulate emulsification in a high-pressure homogenizer for 3 times. Observed under a microscope, most of the emulsion droplet diameter is below 1 micron, only about 5% of the particle diameter is 1-2 micron. The emulsion product is collected, filtered under pressure, and the filter membrane has a pore size of 3 microns. The emulsion was ...

Embodiment 2

[0025] Embodiment Two Bifendate Emulsion No. 2

[0026]Bifendate 5.0g

[0027] Corn Oil 200g

[0028] Tween 80 25g

[0029] Poloxamer P188 10g

[0030] Glyceryl monostearate 10g

[0031] Sodium deoxycholate 5g

[0032] Propylene glycol 3g

[0033] Proper amount of vanillin

[0034] Deionized water up to 1000ml

[0035] The preparation process is close to the examples. Heat the prescribed amount of bifendate, corn oil, Tween 80, poloxamer P188, and glyceryl monostearate to 80°C, and take sodium deoxycholate, vanillin and propylene glycol dissolved in 80°C Add 500ml of deionized water to the tissue masher together, and stir at high speed, 8000 rpm, for 3 minutes each time, repeat 3 times to obtain a white emulsion. After the emulsion is cooled, add deionized water to 1000ml, and circulate emulsification in a high-pressure homogenizer for 3 times. 90% of emulsion droplet diameters are ...

Embodiment 3

[0037] Embodiment No. 1 biphenyl diester oil agent

[0038] Bifendate 2.0g

[0039] Ethyl Oleate 15g

[0040] Tween 80 15g

[0041] Poloxamer P188 5g

[0042] Propylene glycol 5g

[0043] Heat bifendate, ethyl oleate, Tween 80, poloxamer and propylene glycol together to 70°C, after they are all dissolved, cool to room temperature, fill in capsules, 0.42g / capsule, equivalent to Capsules contain 20mg bifendate. Put the capsule in 100ml of water at 37°C, stir slightly, and quickly disperse into an emulsion.

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PUM

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Abstract

A composite liquid biphenyl dimethyl dicarboxylate and its emulsion and oil injections for intravenous injection, intramuscular injection, or oral application are disclosed. Said emulsion has high stability and low granularity. Said solution-type oil has slow releasing effect.

Description

technical field [0001] The invention relates to a fat-containing bifendate liquid pharmaceutical composition, and the dosage forms include emulsion and oil. Background technique [0002] The chemical name of bifendate is 4,4-dimethoxy-5,6,5',6'-dimethoxy-2,2'-dicarboxylate biphenyl. Bifendate is an enzyme-lowering drug for the treatment of hepatitis created in my country, and it is an intermediate in the synthesis of Schisandra C. Oral administration of 150-200 mg / kg of bifendate in mice can alleviate liver damage and elevation of alanine aminotransferase (ALT) caused by carbon tetrachloride. It can inhibit the liver microsomal lipid peroxidation caused by carbon tetrachloride and the metabolic conversion of carbon tetrachloride into carbon monoxide, and reduce the consumption of reduced coenzyme II and oxygen in the metabolic process of carbon tetrachloride, thereby protecting liver cells Structure and function of biofilms. The drug can also reduce prednisone-induced hep...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/216A61K47/44A61P1/16A61P31/12
Inventor 佟丽袁雪莲
Owner 佟丽
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